Literature DB >> 15634025

2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.

Florencio Zaragoza1, Henrik Stephensen, Bernd Peschke, Karin Rimvall.   

Abstract

With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, a series of 2-(4-alkylpiperazin-1-yl)quinolines was prepared. Systematic variation of the substituents led to highly potent histamine H(3) antagonists with low polar surface area and appropriate log P for blood-brain barrier penetration.

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Year:  2005        PMID： 15634025     DOI： 10.1021/jm040873u

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  4 in total

1.  Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.

Authors:  Julien Pedron; Clotilde Boudot; Sébastien Hutter; Sandra Bourgeade-Delmas; Jean-Luc Stigliani; Alix Sournia-Saquet; Alain Moreau; Elisa Boutet-Robinet; Lucie Paloque; Emmanuelle Mothes; Michèle Laget; Laure Vendier; Geneviève Pratviel; Susan Wyllie; Alan Fairlamb; Nadine Azas; Bertrand Courtioux; Alexis Valentin; Pierre Verhaeghe
Journal:  Eur J Med Chem       Date:  2018-06-05       Impact factor: 6.514

2.  Histamine H3-receptor agonists and imidazole-based H3-receptor antagonists can be thermodynamically discriminated.

Authors:  E A Harper; J W Black
Journal:  Br J Pharmacol       Date:  2007-04-02       Impact factor: 8.739

3.  Brønsted acid mediated cyclization of enaminones. Rapid and efficient access to the tetracyclic framework of the Strychnos alkaloids.

Authors:  Rahul V Edwankar; Chitra R Edwankar; Ojas A Namjoshi; Jeffrey R Deschamps; James M Cook
Journal:  J Nat Prod       Date:  2012-01-18       Impact factor: 4.050

4.  New 8-Nitroquinolinone Derivative Displaying Submicromolar in Vitro Activities against Both Trypanosoma brucei and cruzi.

Authors:  Julien Pedron; Clotilde Boudot; Jean-Yves Brossas; Emilie Pinault; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Elisa Boutet-Robinet; Alexandre Destere; Antoine Tronnet; Justine Bergé; Colin Bonduelle; Céline Deraeve; Geneviève Pratviel; Jean-Luc Stigliani; Luc Paris; Dominique Mazier; Sophie Corvaisier; Marc Since; Aurélie Malzert-Fréon; Susan Wyllie; Rachel Milne; Alan H Fairlamb; Alexis Valentin; Bertrand Courtioux; Pierre Verhaeghe
Journal:  ACS Med Chem Lett       Date:  2020-02-06       Impact factor: 4.345
  4 in total

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